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Chemical Structure : CD161
Catalog No.: PC-61129Not For Human Use, Lab Use Only.
CD161 (NKR-P1A) is a potent, selective, orally bioavailable BET bromodomain inhibitor with IC50 of 7.2 and 28.2 nM for BRD4 BD2 and BRD4 BD1, respectively.
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CD161 (NKR-P1A) is a potent, selective, orally bioavailable BET bromodomain inhibitor with IC50 of 7.2 and 28.2 nM for BRD4 BD2 and BRD4 BD1, respectively.
CD161 shows high affinity for BRD2, BRD3, BRD4 and BRDT bromodomains, and liitle to no affintiy for other bromodomains (Ki>500 nM).
CD161 exhibits cytotoxicity against a panel of breast cancer cell lines (MDA-MB-231 IC50=244 nM).
CD161 demonstrates significant antitumor activity in the MV4;11 leukemia and MDA-MB-231 triple-negative breast cancer xenograft models in mice, has excellent microsomal stability and good oral pharmacokinetics in rats and mice.
| M.Wt | 435.487 | |
| Formula | C26H21N5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Zhao Y, et al. J Med Chem. 2017 May 11;60(9):3887-3901.
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